Target
Disintegrin and metalloproteinase domain-containing protein 17
Ligand
BDBM26563
Substrate
TACE substrate peptide
Meas. Tech.
Enzyme Inhibition Assay
pH
7.5±n/a
Temperature
298.15±n/a K
IC50
1±n/a nM
Citation
 Lu, ZOtt, GRAnand, RLiu, RQCovington, MBVaddi, KQian, MNewton, RCChrist, DDTrzaskos, JDuan, JJ Potent, selective, orally bioavailable inhibitors of tumor necrosis factor-alpha converting enzyme (TACE): discovery of indole, benzofuran, imidazopyridine and pyrazolopyridine P1' substituents. Bioorg Med Chem Lett 18:1958-62 (2008) [PubMed]  Article 
Target
Name:
Disintegrin and metalloproteinase domain-containing protein 17
Synonyms:
A disintegrin and metalloproteinase domain 17 | ADA17_PIG | ADAM 17 | ADAM17 | Snake venom-like protease | TACE | TNF-alpha-Converting Enzyme
Type:
Metalloprotease
Mol. Mass.:
12197.99
Organism:
Sus scrofa (pig)
Description:
Partially purified TACE was obtained from porcine spleen.
Residue:
112
Sequence:
MLREQFSFDIAEEASKVCLAHLFTYQDFDMGTLGLAYVGSPRANSHGGVCPKAYYSPIGKKNIYLNSGLTSTKNYGKTILTKEADLVTTHELGHNFGAEHDPDGLAECAPNE
  
Inhibitor
Name:
BDBM26563
Synonyms:
(3R,4R)-4-N-{4-[(2-ethyl-1H-indol-3-yl)methyl]benzene}-3-N-hydroxyoxane-3,4-dicarboxamide | 2-ethyl indole, 19
Type:
Small organic molecule
Emp. Form.:
C24H27N3O4
Mol. Mass.:
421.4889
SMILES:
CCc1[nH]c2ccccc2c1Cc1ccc(cc1)C(=O)N[C@@H]1CCOC[C@@H]1C(=O)NO |r|
Structure:
Search PDB for entries with ligand similarity:
Substrate
Name:
TACE substrate peptide
Synonyms:
n/a
Type:
Internally quenched peptide
Mol. Mass.:
4119.10
Organism:
n/a
Description:
MCA, (7-methoxycoumarin-4-yl)acetyl. Dpa, N-3-(2,4-dinitrophenyl)-L-2,3-diaminopropionyl.
Residue:
39
Sequence:
MCAPRLEALAGLNALAVALDPAARGSERSERSERARGNH